Electrophysiological and receptor binding studies show that the benaodiazepines alter neuronal inhibition in the central nervous system through a GABA receptor/benzodiazepine/ionopore complex. Studies on the pharmacological implications for this complex interaction including GABAergic agents and anticonvulsants are described. In addition, studies on the membrane environment and the biochemical characterization of the isolated benzodiazepine binding site have been carried out.